Composition for cosmetic, pharmaceutical or dietetic use based on an amino sugar and/or a polyhydroxylic acid

ABSTRACT

A composition for cosmetic, pharmaceutical or dietetic use and including as the active ingredient, at least one of the substances which include acetylglucosamine and glucuronic acid in combination with the active ingredients which belong to the chemical class of the carboxylic acids, α-hydroxy acids, vitamins, amino acids, and bioflavonoids, and formulated with particular synergists, additives, and excipients for external use or for internal use.

SUMMARY AND OBJECTS OF THE INVENTION

The object of the present invention is a novel composition for cosmetic,pharmaceutical or dietetic use that is essentially intended for externaluse to be applied either on intact or injured skin, or on the mucousmembranes, and for internal use, taken in the form of tablets,delayed-action tablets, capsules, syrup, drops, suppositories or in anyother pharmaceutical form intended for the taking of the drug orally, orinjected intramuscularly, intravenously, subcutaneously,intra-articularly or in any other form intended for the administrationof the composition in question by means of injection.

More specifically, the present invention pertains to a composition forthe above-mentioned use, which is characterized in that it contains, asthe active ingredient, at least one of the substances which includeacetylglucosamine and glucuronic acid in combination with the activeingredients which belong to the chemical class of the carboxylic acids,α-hydroxy acids, vitamins, amino acids, and bioflavonoids, andformulated with particular synergists, additives, and excipients forexternal use or for internal use.

Acetylglucosamine and glucuronic acid may, by way of indication, also bedescribed as precursors of the glycosaminoglycans. As used herein, theterm glucuronic acid includes both glucuronic acid itself and glucuronicacid lactone as the corresponding cyclized form thereof.

The stimulation of the biosynthesis or even the simple supply ofsuitable biochemical precursors, which may be described, from a purelychemical point of view, as molecular elements that, alone or combined,constitute the monomers or the parts of the monomers of the variouspolysaccharide structures, specifically the glycosaminoglycans, whichcan constitute the polysaccharide fraction of the proteoglycanstructures, produces beneficial biological effects on the treatment ofthe skin against the effects of aging and for the course of treatment ofthe various conditions of the skin, of the joints, and the like.

The purpose of the present invention is precisely to provide a cosmetic,pharmaceutical, or dietetic composition, which is able to develop and tosustain even such biological effects, among others, containing mainlyacetylglucosamine and glucuronic acid in combination with the activeingredients belonging to the chemical class of the carboxylic acids,α-hydroxy acids, vitamins, amino acids, flavonoids, and polysaccharides.

By way of indication, the effects that may be achieved are direct andare expressed as:

biological, physiological, chemical, physical, pharmacological action bythe acetylglucosamine and the glucuronic acid either alone or combined;

a biological, physiological, chemical, physical, or pharmacologicalaction of the polysaccharide and/or proteoglycan molecular structuresobtained by means of the stimulation of the endogenous biosynthesisstarting from the molecular structures of the acetylglucosamine and ofthe glucuronic acid, either alone or combined;

or the effects are indirect and are expressed as:

biological, physiological, chemical, physical, or pharmacological actionof the polysaccharide molecular structures obtained by means of thestimulation of the endogenous biosynthesis of the molecular structuresof the glycosaminoglycans and of the proteoglycans, with other molecularor macromolecular structures present in the human body with which theywould or may interact.

For their synthesis, some glycosaminoglycans have an active metabolitethat is basically represented by UDP-N-acetylglucosamine, which has aprecursor in acetylglucosamine.

Acetylglucosamine belongs to the class of amino sugars, and iswidespread in nature in the form of repetitive polymers of the samemolecular unit to form complex structures, such as chitin, andconstitutes one of the two molecular fractions which form the monomer ofthe various glycosaminoglycans, including hyaluronic acid.

Glucuronic acid, joined with acetylglucosamine by a 1-4-β-glycosidicbond, forms the monomer of hyaluronic acid.

Thus, glucuronic acid acts as a precursor of hyaluronic acid eitheralone or combined with the acetylglucosamine.

Acetylglucosamine and glucuronic acid have the property of preventingthe hyperoxidative phenomena, which, among other things, may have aneffect on the macromolecules of a polysaccharide nature, e.g., thehyaluronic acid.

However, by way of indication and not exhaustively, the action exertedby the acetylglucosamine and by the glucuronic acid towards thestimulation of the biosynthesis of the glycosaminoglycans and theproteoglycans and, consequently, the multiphasic and multicentric actionof the identical glycosaminoglycans and proteoglycans on the skin, onthe joint zones and on the other organic regions are combined.

The therapeutic role played by acetylglucosamine, by glucuronic acid,and by their interaction thus appears to be clear in all thosepathological forms, in which it becomes necessary to stimulate theendogenous production, e.g., of hyaluronic acid.

In the field of cosmetics, since a reduction in the amount of hyaluronicacid present in the skin occurs during aging, with resulting dehydrationof the skin, appearance of wrinkles and loss of elasticity and oftonicity of the skin, the action exerted by acetylglucosamine, byglucuronic acid and by the related combination is of considerableimportance.

In addition, the action of the glycosaminoglycans, whose production maybe stimulated by the acetylglucosamine and by the glucuronic acid,either alone or combined, also involves, among other things, the otherstructures of the skin, such as the collagens, the elastic fibers, andthe structural proteins, so that a stimulation by means of theabove-mentioned biochemical precursors of the glycosaminoglycans and ofthe proteoglycans of the amorphous matrix of the skin leads toaesthetically and pharmacologically relevant results.

The action exerted by the acetylglucosamine and by glucuronic acid,either alone or combined, with other active ingredients of a flavonoidnature either in the pure form or contained in extracts of plants orfruits or of parts of plants also proves to be particularly important infighting against the problems which are associated with the biological,physiological, as well as physiopathological or pathological regressionof the circulation and of the microcirculation.

In fact, it appears to be justified to consider, besides parietalfactors, the existence of extraparietal factors, which may interferewith many functional aspects of the wall of a vessel, both inphysiological conditions and especially in pathological conditions.

In fact, it is fair to believe that not only the permeability of thesmall vessels, but also the parietal reactive aspects are conditioned bythe molecular integrity of complex glycosaminoglycans and/orproteoglycans of the perivascular interstitium.

The action that is exerted by the acetylglucosamine and by glucuronicacid with other active ingredients belonging to the class of eithermonocarboxylic or bicarboxylic α-hydroxy acids also proves to beparticularly important in improving the conditions of skin hydrationeither in the presence of changes of a physiological nature or of aphysiopathological or pathological nature.

In case of application for topical use, the keratolytic action exertedby the promotes the absorption of the acetylglucosamine and of theglucuronic acid, making possible a better bioavailability of the twoactive ingredients and thus a more marked stimulating action on thebiosynthesis of the glycosaminoglycans.

The combination of acetylglucosamine and glucuronic acid with hyaluronicacid (in the polymer form) also proves to be particularly positive inthe case of subcutaneous or intradermal use.

In fact, the use of hyaluronic acid injected in the dermis, thanks toits property of holding considerable amounts of water, makes it possibleto raise the skin, reducing the presence of wrinkles thanks to aphysical type action.

Since the hyaluronic acid injected intradermally is degraded inrelatively short times, the endogenous, stimulating action of hyaluronicacid performed by acetylglucosamine and by glucuronic acid appears to bejustified.

The various features of novelty which characterize the invention arepointed out with particularity in the claims annexed to and forming apart of this disclosure. For a better understanding of the invention,its operating advantages and specific objects attained by its uses,reference is made to the accompanying descriptive matter in whichpreferred embodiments of the invention are illustrated.

DESCRIPTION OF THE PREFERRED EMBODIMENT

When used alone, the acetylglucosamine may be contained in thecomposition in an amount of 0.01 to 30 wt. %, and preferably from 0.05to 15 wt. %, based on the final formulation.

When used alone, the glucuronic acid may be contained in the compositionin an amount of 0.001 to 20 wt. %, and preferably from 0.05 to 30 wt. %,based on the final formulation.

When used combined, the acetylglucosamine and the glucuronic acid (orthe glucuronolactone) may be contained in the composition in an amountof 0.0001 to 50 wt. % each, and preferably in an amount equal to 0.05 to15 wt. % each.

In addition, the composition based on acetylglucosamine and/orglucuronic acid may contain various active ingredients, which we willdefine as synergists for descriptive simplicity.

The synergists may be selected from the group comprising carboxylicacids, α-hydroxy acids and β-hydroxy acids, either monocarboxylic orbicarboxylic.

Glycolic acid, lactic acid, hydroxybutyric acid, mandelic acid, tartaricacid, malic acid, salicylic acid, hydroxybenzoic acid, citric acid,lipoic acid (thioctic acid), either in the oxidized or reduced form,intended both in the dextrorotatory and levorotatory forms, as well asthe racemic mixtures and the corresponding salts, esters or amides, maybe mentioned as examples.

Two or more of these synergists may be present in the composition, aloneor combined, together with the acetylglucosamine and/or the glucuronicacid.

Such synergists may be contained in amounts ranging from 0.001 to 50 wt.%, and preferably from 0.5 to 15 wt. %, based on the final formulationwhen the proportions of the acetylglucosamine and/or of the glucuronicacid are each 0.05 to 15 wt. %.

In addition, the composition of the present invention may contain eitherliposoluble or water-soluble vitamins.

Examples are: vitamin B1 (or thiamin), vitamin B2 (riboflavin), vitaminB6 (or pyridoxine, pyridoxal, pyridoxamine), niacin (nicotinic acid,nicotinic amide), pantothenic acid, biotin, folic acid (folic acid,folinic acid), vitamin E (tocopherol), vitamin C (ascorbic acid), betacarotene, retinol (vitamin A), retinal, retinoic acid, para-aminobenzoicacid (4-aminobenzoic acid), vitamin F (linoleic acid), vitamin F(linolenic acid), vitamin F (arachidonic acid), vitamin P (rutin), inboth the dextrorotatory and levorotatory forms, as well as the relatedracemic mixtures, and the corresponding salts or esters in the variousweight ratios described below.

When present, these substances may be contained in amounts of 0.001 to10 wt. %, and preferably of 0.05 to 1 wt. % when the proportions ofacetylglucosamine and/or glucuronic acid are each from 0.05 to 15 wt. %.

The composition of the present invention may also contain plants,extracts of plant or parts of plants or their extracts, including roots,leaves, fruits, bark, flowering top, in the form of dry, soft or liquidextracts.

The following may be mentioned as examples of these synergists: SilybumMarianum, Echinacea Angustifolia, Aesculus Hippocsatanum, CalendulaOfficinalis, Centella Asiatica, Hamamelis Virginiana Vaccinum Myrtillus,Citrus Aurantium Amara, Citrus Aurantium Dulcis, Citrus Limonium,Equisetum Arvense, Glycirrhiza Glabra, Aloe Vera, Ruta Graveolans, VitisVinifera used alone or combined.

The presence of these synergists may be 0.001 to 30 wt. %, andpreferably 0.25 to 20 wt. % when acetylglucosamine and/or glucuronicacid are each contained in amount of 0.05 to 15 wt. %.

The composition of the present invention may also contain, either aloneor in combination, chemical substances that may be terpenes,triterpenes, saponins, isoflavonoids, alcohol flavonoids, and the like.

Anthocyanidins of the bilberry, escin, madecassic acid, madecassosides,asiaticosides, asiatic acid, rutin and its derivatives, including thesalts and esters thereof, diosmin, sericic acid, sericosides,echinacosides, echinacin, glycerretic acid and its salts or esters,quercitin, isoquercitin, bisabolene, silymarin, cyanidins,leucocyanidins, although contained in plant extracts or plant parts(including leaves, roots, fruits, bark) and the corresponding salts oresters, may be mentioned as examples of these substances.

These substances may be contained in an amount of 0.01 to 20 wt. %, andpreferably from 0.05 to 15 wt. %.

The composition of the present invention may contain, alone or combined,substances belonging to the chemical class of amino acids selected fromamong: alanine arginine, aspartic acid, asparagine, cysteine, glutamicacid, glutamine, glycine, histidine, leucine, isoleucine, lysine,methionine, phenylalanine, proline, serine, threonine, tryptophan,tyrosine, valine, the corresponding salts and esters and the variousforms reduced to amino alcohols, both in dextrorotatory and levorotatoryform and the related racemic mixtures.

These substances may be contained in amounts of 0.001 to 20 wt. %, andpreferably from 0.05 to 15 wt. % when the acetylglucosamine and/or theglucuronic acid are each contained in amounts of 0.05 to 15 wt. %.

The composition of the present invention may contain, alone or combined,substances belonging to the chemical class of the polysaccharides,including hyaluronic acid, chitin, chitosan, dermatan sulfate, andheparin. These substances may be contained in amounts of 0.0001 to 20wt. %, and preferably from 0.05 to 5 wt. % when the acetylglucosamineand/or the glucuronic acid are each contained in amounts of 0.05 to 15wt. %.

The combination of acetylglucosamine, of glucuronic acid, or of bothwith suitable synergists proves to be innovative in the field ofcosmetics in dealing with various phenomena associated with thedegeneration of aesthetic parameters of the skin. It is particularlyuseful, but not exclusively, for a moisturizing action, an anti-agingaction, anti-wrinkle action, elasticizing action, hardening action,anti-cellulitis action, the cosmetic treatment of baldness, the cosmetictreatment of teleangectasia and of blotchiness.

Its use is also innovative in the pharmaceutical field for the topicaltreatment of atopic dermatitides, seborrheic dermatitides, nummulareczematous dermatitides, exfoliative dermatitides, stasis dermatitides,neurodermatitides, acne, acne rosacea, cicatricial alopecia, hippocraticalopecia, female-pattern alopecia, drug-induced alopecia, alopeciaareata, pseudofolliculitis, psoriasis, lichen ruber planus, ichthyosis,xeroderma, keratosis pilaris, decubitus ulcers, trophic ulcers, torpidsores, vascular spider angiomas, hemangiomas, telangiectatic granuloma,seborrheic keratosis, fibrous histiocytoma, morphea, the treatment ofhypertrophic scars, burn scars, teleangectasia, changes in thecirculation and the microcirculation, venous stasis, circulatory stasis,lupus erythematosus, topical treatment of scleroderma, and healing ofwounds.

The composition of the present invention, which containsacetylglucosamine and/or glucuronic acid optionally with other activeingredients, vitamins, and various additives, may be prepared informulations for external use, as water-in-oil emulsions, oil-in-wateremulsions, monophasic solutions, biphasic pseudo solutions, monophasicgels, biphasic gels or submicellar gels, anhydrous salves, dustingpowders, etc., or for internal use, as capsules, tablets, drops, syrups,intramuscular, intravenous, subcutaneous, or intra-articular injections,etc., using the appropriate supports or vehicles.

The composition of the present invention may also be effectively usedfor internal use in the pharmaceutical field, e.g., in the treatment ofdegenerative forms of the amorphous component of tissues, circulatorystasis, venous stasis, rheumatoid arthritis, osteoarthritis, arthrosis,scleroderma, etc.

The following preparation examples are further illustrative of and, inthe cases specified, descriptive of the composition of the presentinvention.

In these examples, the proportions, if not indicated otherwise, are inweight percent based on the final composition.

THE USE OF THE COMPOSITION IN THE FORM OF AN EMULSION OBTAINED BY MEANSOF PREPARATION EXAMPLE 1

(Cosmetic and/or Pharmaceutical Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid and Diosmin

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with deficits of a circulatory natureeither in the veins or in the microcirculation (capillaries), which canbe used either in the pharmaceutical field or in the field of cosmetics(by way of indication, but not exhaustively, for the treatment ofliposclerosis, commonly defined cellulitis, heaviness of the legs,teleangectasias of various origins and locations).

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, described below together withtypes of ingredients used, makes it possible to obtain a mesomorphicphase, in which a multilamellar, crystalline liquid phase with themolecular property of the solid phase and the mobility property of theliquid phase is formed on the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid and diosmin, which are structured in a multilamellar-based,crystalline liquid emulsion, represents an innovation that is able toyield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                           Amount in wt. %                                                               From  to                                                   ______________________________________                                            PHASE (A)                                                                 1.               STEARETH-2                                                                                  0.500                                                                                         4.000 (x)                      2.       CETEARYL GLUCOSIDE                                                                                  0.200                                                                                         6.000 (x)                      3.     PPG-15-STEARYL ETHER                                                                                  6.000                                                                                    12.500 (y)                          4.              STEARETH-21                                                                                  0.100                                                                                         6.400 (x)                      5.            CETYL ALCOHOL                                                                                  0.750                                                                                         6.100 (y)                      6.             STEARIC ACID                                                                                  0.100                                                                                         7.800 (y)                      7.         CETEARYL ALCOHOL                                                                                  0.100                                                                                         5.600 (y)                      8.       CETEARYL OCTANOATE                                                                                  0.200                                                                                         4.000 (y)                      9.  PHASE (B)                                                                 10.       ACETYLGLUCOSAMINE                                                                                  0.100                                                                                 7.900                                  11. D-GLUCURONIC ACID GAMMA                                                                                  0.100                                                                                 7.900                                                      LACTONE                                                   12.               WATER qs.                                                                                  5.000                                                                                 5.000                                  13. PHASE (C)                                                                 14.                 DIOSMIN                                                                                  0.100                                                                                 4.750                                  15.               WATER qs.                                                                                    100                                                                           100                                          ______________________________________                                    

Method of Preparation:

1. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

2. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

3. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

4. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

5. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

PREPARATION EXAMPLE 2

(Cosmetic Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid and Silymarin, Tocopherol

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with the typical problems of skin,which is sensitive and can easily turn red, and with problems of theformation of teleangectasias.

The present formulation has a marked antioxidant effect, which is ableto prevent or hinder the phenomena linked with aging of the skin.

The present formulation also proves to be indicated for hindering thesymptoms of acne rosacea, mainly but not exclusively in the initialclinical stages.

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, together with types of ingredientsused, makes it possible to obtain a mesomorphic phase, in which amultilamellar, crystalline liquid phase with the molecular property ofthe solid phase and the mobility property of the liquid phase is formedon the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid, of silymarin and of tocopherol, which are structured in amultilamellar-based, crystalline liquid emulsion, represents aninnovation that is able to yield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                           Amount in wt. %                                                               From  to                                                   ______________________________________                                            PHASE (A)                                                                 1.               STEARETH-2                                                                                  0.500                                                                                         4.000 (x)                      2.       CETEARYL GLUCOSIDE                                                                                  0.200                                                                                         6.000 (x)                      3.     PPG-15-STEARYL ETHER                                                                                  6.000                                                                                    12.500 (y)                          4.              STEARETH-21                                                                                  0.100                                                                                         6.400 (x)                      5.            CETYL ALCOHOL                                                                                  0.750                                                                                         6.100 (y)                      6.             STEARIC ACID                                                                                  0.100                                                                                         7.800 (y)                      7.         CETEARYL ALCOHOL                                                                                  0.100                                                                                         5.600 (y)                      8.       CETEARYL OCTANOATE                                                                                  0.200                                                                                         4.000 (y)                      9.       TOCOPHERYL ACETATE                                                                                  0.100                                                                                 7.000                                  10. PHASE (B)                                                                 11.       ACETYLGLUCOSAMINE                                                                                  0.100                                                                                 7.900                                  12. D-GLUCURONIC ACID GAMMA                                                                                  0.100                                                                                 7.900                                                      LACTONE                                                   13.               WATER qs.                                                                                  5.000                                                                                 5.000                                  14. PHASE (C)                                                                 15.               SILYMARIN                                                                                  0.100                                                                                 4.750                                  16.               WATER qs.                                                                                    100                                                                           100                                          ______________________________________                                    

Method of Preparation:

6. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

7. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

8. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

9. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

10. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

PREPARATION EXAMPLE 3

(Cosmetic and/or Pharmaceutical Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid, Asiatic Acid, Proline

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with the degeneration of the elasticcharacteristics of the skin.

The present formulation has an effect that is able to hinder theformation of hypertrophic scars and keloids.

The present formulation also proves to be indicated for improving thehealing of skin lesions.

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, together with types of ingredientsused, makes it possible to obtain a mesomorphic phase, in which amultilamellar, crystalline liquid phase with the molecular property ofthe solid phase and the mobility property of the liquid phase is formedon the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid, of proline, and of asiatic acid, which are structured in amultilamellar-based, crystalline liquid emulsion, represents aninnovation that is able to yield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                           Amount in wt. %                                                               From  to                                                   ______________________________________                                            PHASE (A)                                                                 1.               STEARETH-2                                                                                  0.500                                                                                         4.000 (x)                      2.       CETEARYL GLUCOSIDE                                                                                  0.200                                                                                         6.000 (x)                      3.     PPG-15-STEARYL ETHER                                                                                  6.000                                                                                    12.500 (y)                          4.              STEARETH-21                                                                                  0.100                                                                                         6.400 (x)                      5.            CETYL ALCOHOL                                                                                  0.750                                                                                         6.100 (y)                      6.             STEARIC ACID                                                                                  0.100                                                                                         7.800 (y)                      7.         CETEARYL ALCOHOL                                                                                  0.100                                                                                         5.600 (y)                      8.       CETEARYL OCTANOATE                                                                                  0.200                                                                                         4.000 (y)                      9.  PHASE (B)                                                                 10.       ACETYLGLUCOSAMINE                                                                                  0.100                                                                                 7.900                                  11. D-GLUCURONIC ACID GAMMA                                                                                  0.100                                                                                 7.900                                                      LACTONE                                                   12.                 PROLINE                                                                                  0.050                                                                                 6.000                                  13.               WATER qs.                                                                                  5.000                                                                                 5.000                                  14. PHASE (C)                                                                 15.            ASIATIC ACID                                                                                  0.010                                                                                 4.750                                  16.        PROPYLENE GLYCOL                                                                                  2.000                                                                                 6.000                                  17.               WATER qs.                                                                                    100                                                                           100                                          ______________________________________                                    

Method of Preparation:

11. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

12. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

13. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

14. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

15. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

PREPARATION EXAMPLE 4

(Cosmetic and/or Pharmaceutical Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid, Sericic Acid

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with the healing process of a woundand/or of a sore.

The present formulation has a marked effect that is able to improve theaesthetic quality of the scar.

The present formulation proves to be indicated for protecting the scarfrom the damages caused by solar radiation if either chemical orphysical sun filters are added to the formulation.

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, together with types of ingredientsused, makes it possible to obtain a mesomorphic phase, in which amultilamellar, crystalline liquid phase with the molecular property ofthe solid phase and the mobility property of the liquid phase is formedon the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid, and of sericic acid, which are structured in amultilamellar-based, crystalline liquid emulsion, represents aninnovation that is able to yield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                           Amount in wt. %                                                               From  to                                                   ______________________________________                                            PHASE (A)                                                                 2.               STEARETH-2                                                                                  0.500                                                                                         4.000 (x)                      3.       CETEARYL GLUCOSIDE                                                                                  0.200                                                                                         6.000 (x)                      4.     PPG-15-STEARYL ETHER                                                                                  6.000                                                                                    12.500 (y)                          5.              STEARETH-21                                                                                  0.100                                                                                         6.400 (x)                      6.            CETYL ALCOHOL                                                                                  0.750                                                                                         6.100 (y)                      7.             STEARIC ACID                                                                                  0.100                                                                                         7.800 (y)                      8.         CETEARYL ALCOHOL                                                                                  0.100                                                                                         5.600 (y)                      9.       CETEARYL OCTANOATE                                                                                  0.200                                                                                         4.000 (y)                      10.        TITANIUM DIOXIDE                                                                                 10.000                                                                            35.000                                          PHASE (B)                                                                 11.       ACETYLGLUCOSAMINE                                                                                  0.100                                                                                 7.900                                  12. D-GLUCURONIC ACID GAMMA                                                                                  0.100                                                                                 7.900                                                      LACTONE                                                   13.               WATER qs.                                                                                  5.000                                                                                 5.000                                      PHASE (C)                                                                 14.            SERICIC ACID                                                                                  0.010                                                                                 6.750                                  15.               WATER qs.                                                                                    100                                                                           100                                          ______________________________________                                    

Method of Preparation:

1. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

2. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

3. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

4. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

5. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

PREPARATION EXAMPLE 5

(Cosmetic Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid, Retinol, Tocopherol

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with the aging of the skin.

The present formulation has a marked antioxidant effect that is able toprevent or hinder the formation of wrinkles.

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, together with types of ingredientsused, makes it possible to obtain a mesomorphic phase, in which amultilamellar, crystalline liquid phase with the molecular property ofthe solid phase and the mobility property of the liquid phase is formedon the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid, of retinol and of tocopherol, which are structured in amultilamellar-based, crystalline liquid emulsion, represents aninnovation that is able to yield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                            Amount in wt. %                                                               From  to                                                  ______________________________________                                            PHASE (A)                                                                 1.                              0.5002                                                                                        4.000 (x)                     2.                  CETEARYL GLUCOSIDE                                                                        0.200                                                                                         6.000 (x)                     3.                PPG-15-STEARYL ETHER                                                                        6.000                                                                                    12.500 (y)                         4.                              0.1001                                                                                        6.400 (x)                     5.                       CETYL ALCOHOL                                                                        0.750                                                                                         6.100 (y)                     6.                        STEARIC ACID                                                                        0.100                                                                                         7.800 (y)                     7.                    CETEARYL ALCOHOL                                                                        0.100                                                                                         5.600 (y)                     8.                  CETEARYL OCTANOATE                                                                        0.200                                                                                         4.000 (y)                     9.  RETINYL PALMITATE (1,000,000 IU/g)                                                                        0.050                                                                                 4.000                                 10.                 TOCOPHERYL ACETATE                                                                        0.075                                                                            10.000                                         PHASE (B)                                                                 11.                  ACETYLGLUCOSAMINE                                                                        0.100                                                                                 7.900                                 12.            D-GLUCURONIC ACID GAMMA                                                                        0.100                                                                                 7.900                                                                LACTONE                                        13.                             5.000.                                                                                5.000                                     PHASE (C)                                                                 14.                             0.100L                                                                                8.750                                 15.                               100.                                                                          100                                         ______________________________________                                    

Method of Preparation:

16. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

17. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

18. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

19. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

20. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

PREPARATION EXAMPLE 5

(Cosmetic Use)

Multilamellar-based, Crystalline, Liquid Emulsion ContainingAcetylglucosamine, Glucuronic Acid, Glycolic Acid

This is a structured oil-in-water emulsion in the form of amultilamellar, crystalline, liquid phase, which is mainly indicated todeal with the problems associated with the aging of the skin and withdehydration of the skin.

The present formulation has a marked moisturizing effect and, in case ofusing high doses of glycolic acid, is able to prevent or hinder theformation of wrinkles by means of a marked exfoliating action andchemical peeling.

The action exerted by the glycolic acid also promotes the penetrationinto the skin both of the acetylglucosamine and of the glucuronic acid,thus making possible a synchronized action that is able to yieldappreciable clinical and aesthetic results.

The formation of the multilamellar, crystalline liquid phase inside theemulsion is obtained by means of an accurate calibration of a ternarysystem (x) and by a pentenary system (y), which are represented by threecetyl or stearyl type emulsifying agents and by five chemical entitiesof a lipid nature, either solid or liquid, also cetyl or stearyl type,respectively.

The particular method of preparation, together with types of ingredientsused, makes it possible to obtain a mesomorphic phase, in which amultilamellar, crystalline liquid phase with the molecular property ofthe solid phase and the mobility property of the liquid phase is formedon the surface of the oil micelles.

This particular chemical-physical configuration of the emulsion provesto be visible by means of analysis using polarized-light microscopy.

The structured emulsion in the form of a multilamellar, crystallineliquid phase makes it possible to amplify the action of the product overtime, to act as a "reservoir" of active ingredients, proves to be usefulin the protection of the active ingredients used, and increases thestability of the emulsion.

Thus, the calibrated combination of acetylglucosamine, of glucuronicacid, and of glycolic acid, which are structured in amultilamellar-based, crystalline liquid emulsion, represents aninnovation that is able to yield remarkable results.

Water-in-oil Emulsion

    ______________________________________                                                            Amount in wt. %                                                               From  to                                                  ______________________________________                                            PHASE (A)                                                                 16.                             0.5002                                                                                        4.000 (x)                     17.                 CETEARYL GLUCOSIDE                                                                        0.200                                                                                         6.000 (x)                     18.               PPG-15-STEARYL ETHER                                                                        6.000                                                                                    12.500 (y)                         19.                             0.1001                                                                                        6.400 (x)                     20.                      CETYL ALCOHOL                                                                        0.750                                                                                         6.100 (y)                     21.                       STEARIC ACID                                                                        0.100                                                                                         7.800 (y)                     22.                   CETEARYL ALCOHOL                                                                        0.100                                                                                         5.600 (y)                     23.                 CETEARYL OCTANOATE                                                                        0.200                                                                                         4.000 (y)                     24. RETINYL PALMITATE (1,000,000 IU/g)                                                                        0.050                                                                                 4.000                                 25.                 TOCOPHERYL ACETATE                                                                        0.075                                                                            10.000                                         PHASE (B)                                                                 26.                  ACETYLGLUCOSAMINE                                                                        0.100                                                                                 7.900                                 27.            D-GLUCURONIC ACID GAMMA                                                                        0.100                                                                                 7.900                                                                LACTONE                                        28.                             5.000.                                                                                5.000                                     PHASE (C)                                                                 29.                             0.100L                                                                                8.750                                 30.                               100.                                                                          100                                         ______________________________________                                    

Method of Preparation:

21. Heat phase A) to +80° C. and then heat phase C) to +72° C. Combinephase C) with phase A) and homogenize for 15 minutes at 2,500 rpm, underagitation and aspirated vacuum.

22. Initiate a slow cooling with a reduction of 2.5° C. every 4 minutes.

23. At +45° C., homogenize at 3,000 rpm for 7 minutes continually underagitation.

24. At +40° C., add phase B) under agitation and allow to cool to atemperature of 30° C., continually under agitation.

25. Upon reaching 30° C., homogenize for 10 minutes at 2,000 rpm.

Preparation for Pharmaceutical Use

Pharmaceutical Form: Vial for intradermal injection

    ______________________________________                                                           From   to                                                  ______________________________________                                        1.    ACETYLGLUCOSAMINE  0.0010   2.500                                       2.    GLUCURONIC ACID                    2.500                                3.    HYALURONIC ACID                    50.00                                4.    PHYSIOLOGICAL WATER qs.                                                                                            100                                5.    PRESERVATIVE qs.                                                        ______________________________________                                    

Method of Preparation

Dissolve 1.+2.+5. in 4. Add 3. to the solution obtained. Allow tosolvate until a clear gel is obtained. Sterilize and then package invial.

Preparation for Pharmaceutical Use in Capsules or Tablets

Composition per Unit of Administration

    ______________________________________                                        1.      ACETYLGLUCOSAMINE                                                                              50 mg                                                2.              GLUCURONIC ACID                                                                               50 mg                                         3.                      LACTOSE                                                                               70 mg                                         4.           MAGNESIUM STEARATE                                                                             3 mg                                            ______________________________________                                    

Method of Preparation:

Mix 1+2.+3.+4. after having provided the various ingredients with equalparticle size. Then compress or encapsulate.

Preparation for Pharmaceutical or Dietetic Use

    ______________________________________                                        1.      ACETYLGLUCOSAMINE                                                                              15       mg                                          2.              GLUCURONIC ACID                                                                               15                                                                                     mg                                   3.                LEUCOCYANIDIN                                                                               90                                                                                     mg                                   4.                   TOCOPHEROL                                                                                5                                                                                     mg                                   5.                     SELENIUM                                                                                1                                                                                    mcg                                   6.                      LACTOSE                                                                               50                                                                                     mg                                   7.           MAGNESIUM STEARATE                                                                                2                                                                                     mg                                   ______________________________________                                    

Method of Preparation:

Mix 1.+2.+3.+4.+5.+6.+7. after having provided the various ingredientswith equal particle size. Then compress or encapsulate.

While specific embodiments of the invention have been shown anddescribed in detail to illustrate the application of the principles ofthe invention, it will be understood that the invention may be embodiedotherwise without departing from such principles.

What is claimed is:
 1. Composition for therapeutic cosmetic,pharmaceutical or dietetic use comprising a pharmaceutical vehiclecontaining as active ingredient an effective amount of at least oneindividual compound selected from the group consisting of the individualcompound acetylglucosamine and the individual compound glucuronic acid,and at least one substance selected from the group consisting ofmonocarboxylic acids, dicarboxylic acids, α-hydroxy acids, β-hydroxyacids, plants and extracts thereof, flavonoids, bioflavonoids,isoflavonoids, saponins, terpenes, triterpenes, amino acids,water-soluble vitamins and lipo-soluble vitamins.
 2. Composition ofclaim 1 wherein said substance is at least one acid selected from thegroup consisting of glycolic acid, lactic acid, hydroxybutyric acid,mandelic acid, tartaric acid, malic acid, hydroxybenzoic acid, citricacid, lipoic acid, and the corresponding salts and esters thereof. 3.Composition of claim 1 wherein said substance is at least one vitaminsubstance selected from the group consisting of vitamin B1, vitamin B2,vitamin B6, niacin, pantothenic acid, biotin, folic acid, ascorbic acid,beta carotene, retinol, retinal, retinoic acid, p-aminobenzoic acid,tocopherol and vitamin F.
 4. Composition of claim 1 wherein saidsubstance is at least one plant or extract thereof selected from thegroup consisting of Vaccinum Myrtillus, Sylibum Marianum, EchinaceaAngustifolia, Aesculus Hippocastanum, Calendula Officinalis, CentellaAsiatica, Hamamelis Virginiana, Citrus Aurantium Amara, Citrus AurantiumDulcis, Citrus Limonium, Equisetum Arvense, Glycyrritia Glabbra, AloeVera, Ruta Graveolans, Vitis Vinifera and Terminalia Sericea. 5.Composition of claim 1 wherein said substance is at least one amino acidselected from the group consisting of alanine, arginine, aspartic acid,asparagine, cysteine, glutamic acid, glutamine, glycine, histidine,leucine, isoleucine, lysine, methionine, phenylalanine, proline, serine,threonine, tryptophan, tyrosine, valine, the corresponding salts andesters thereof, and the corresponding amino alcohols thereof. 6.Composition of claim 1 wherein said substance is at least one substanceselected from the group consisting of terpenes, triterpenes, saponins,isoflavonoids, flavonoids and bioflavonoids.
 7. Composition of claim 6wherein said substance is at least one substance selected from the groupconsisting of anthocyanidins of the bilberry, escin, madecassic acid,madecassosides, asiaticosides, asiatic acid, rutin and its derivatives,diosmin, sericic acid, sericosides, echinacosides, echinacin,glycerretic acid, quercitin, isoquercitin, bisabolene, silymarin,cyanidins, leucocyanidins, and the corresponding salts and estersthereof.
 8. Composition for therapeutic cosmetic, pharmaceutical ordietetic use comprising a pharmaceutical vehicle containing as activeingredient an effective amount of at least one individual compoundselected from the group consisting of the individual compoundacetylglucosamine and the individual compound glucuronic acid, and atleast one sulfated or unsulfated polysaccharide selected from the groupconsisting of hyaluronic acid, chitin, dermatan sulfate, heparin, andthe corresponding salts and esters thereof.
 9. Composition fortherapeutic cosmetic, pharmaceutical or dietetic use comprising apharmaceutical vehicle containing as active ingredient an effectiveamount of at least one individual compound selected from the groupconsisting of the individual compound acetylglucosamine and theindividual compound glucuronic acid, and at least one substance selectedfrom the group consisting of diosmin, silymarin, tocopherol, asiaticacid, proline, sericic acid, retinol, glycolic acid, hyaluronic acid andleucocyanidin.
 10. Method of therapeutically treating the skin of asubject against the effects of aging or to promote healing of skininjury or infection comprising administering to the skin of the subjectan effective amount of a composition comprising as active ingredient atleast one individual compound selected from the group consisting of theindividual compound acetylglucosamine and the individual compoundglucuronic acid.
 11. Method of claim 10 wherein the composition furthercomprises at least one substance selected from the group consisting ofmonocarboxylic acids, dicarboxylic acids, α-hydroxy acids, β-hydroxyacids, plants and extracts thereof, flavonoids, bioflavonoids,isoflavonoids, saponins, terpenes, triterpenes, amino acids,water-soluble vitamins and lipo-soluble vitamins.
 12. Method of claim 10wherein the composition further comprises at least one acid selectedfrom the group consisting of glycolic acid, lactic acid, hydroxybutyricacid, mandelic acid, tartaric acid, malic acid, hydroxybenzoic acid,citric acid, lipoic acid, and the corresponding salts and estersthereof.
 13. Method of claim 10 wherein the composition furthercomprises at least one vitamin substance selected from the groupconsisting of vitamin B1, vitamin B2, vitamin B6, niacin, pantothenicacid, biotin, folic acid, ascorbic acid, beta carotene, retinol,retinal, retinoic acid, p-aminobenzoic acid, tocopherol and vitamin F.14. Method of claim 10 wherein the composition further comprises atleast one plant or extract thereof selected from the group consisting ofVaccinum Myrtillus, Sylibum Marianum, Echinacea Angustifolia, AesculusHippocastanum, Calendula Officinalis, Centella Asiatica, HamamelisVirginiana, Citrus Aurantium Amara, Citrus Aurantium Dulcis, CitrusLimonium, Equisetum Arvense, Glycyrritia Glabbra, Aloe Vera, RutaGraveolans, Vitis Vinifera and Terminalia Sericea.
 15. Method of claim10 wherein the composition further comprises at least one amino acidselected from the group consisting of alanine, arginine, aspartic acid,asparagine, cysteine, glutamic acid, glutamine, glycine, histidine,leucine, isoleucine, lysine, methionine, phenylalanine, proline, serine,threonine, tryptophan, tyrosine, valine, the corresponding salts andesters thereof, and the corresponding amino alcohols thereof.
 16. Methodof claim 10 wherein the composition further comprises at least onesubstance selected from the group consisting of terpenes, triterpenes,saponins, isoflavonoids, flavonoids and bioflavonoids.
 17. Method ofclaim 10 wherein the composition further comprises at least onesubstance selected from the group consisting of anthocyanidins of thebilberry, escin, madecassic acid, madecassosides, asiaticosides, asiaticacid, rutin and its derivatives, diosmin, sericic acid, sericosides,echinacosides, echinacin, glycerretic acid, quercitin, isoquercitin,bisabolene, silymarin, cyanidins, leucocyanidins, and the correspondingsalts and esters thereof.
 18. Method of claim 10 wherein the compositionfurther comprises at least one sulfated or unsulfated polysaccharideselected from the group consisting of hyaluronic acid, chitin, dermatansulfate, heparin, and the corresponding salts and esters thereof. 19.Method of claim 10 wherein the composition further comprises at leastone substance selected from the group consisting of diosmin, silymarin,tocopherol, asiatic acid, proline, sericic acid, retinol, glycolic acid,hyaluronic acid and leucocyanidin.
 20. Composition for therapeuticcosmetic, pharmaceutical or dietetic use comprising a pharmaceuticalvehicle containing as active ingredient an effective amount of at leastone individual compound selected from the group consisting of 0.001-30%by weight of the individual compound acetylglucosamine and theindividual compound glucuronic acid.
 21. Composition for therapeuticcosmetic, pharmaceutical or dietetic use comprising a pharmaceuticalvehicle containing as active ingredient an effective amount of at leastone individual compound selected from the group consisting of theindividual compound acetylglucosamine and 0.001-30% by weight of theindividual compound glucuronic acid.
 22. Composition of claim 21 whereinthe individual compound acetylglucosamine and the individual compoundglucuronic acid are present in equimolar amounts.
 23. Composition fortherapeutic cosmetic, pharmaceutical or dietetic use comprising apharmaceutical vehicle containing as active ingredient an effectiveamount of at least one individual compound selected from the groupconsisting of 0.05-10% by weight of the individual compoundacetylglucosamine and 0.05-10% by weight of the individual compoundglucuronic acid.